Details of the Drug Therapeutic Target (DTT)

General Information of Drug Therapeutic Target (DTT) (ID: TTSBVFO)

DTT Name Dual-specificity tyrosine-phosphorylation regulated kinase 1A (DYRK1A)
Synonyms hMNB; Protein kinase minibrain homolog; MNBH; MNB; HP86; Dual specificity tyrosine-phosphorylation-regulated kinase 1A; Dual specificity YAK1-related kinase; DYRK
Gene Name DYRK1A
DTT Type
Patented-recorded target
 [1]
BioChemical Class
Kinase
UniProt ID
DYR1A_HUMAN
TTD ID
T92803
3D Structure
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2D Sequence (FASTA)
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3D Structure (PDB)
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EC Number
EC 2.7.12.1
Sequence
MHTGGETSACKPSSVRLAPSFSFHAAGLQMAGQMPHSHQYSDRRQPNISDQQVSALSYSD
QIQQPLTNQVMPDIVMLQRRMPQTFRDPATAPLRKLSVDLIKTYKHINEVYYAKKKRRHQ
QGQGDDSSHKKERKVYNDGYDDDNYDYIVKNGEKWMDRYEIDSLIGKGSFGQVVKAYDRV
EQEWVAIKIIKNKKAFLNQAQIEVRLLELMNKHDTEMKYYIVHLKRHFMFRNHLCLVFEM
LSYNLYDLLRNTNFRGVSLNLTRKFAQQMCTALLFLATPELSIIHCDLKPENILLCNPKR
SAIKIVDFGSSCQLGQRIYQYIQSRFYRSPEVLLGMPYDLAIDMWSLGCILVEMHTGEPL
FSGANEVDQMNKIVEVLGIPPAHILDQAPKARKFFEKLPDGTWNLKKTKDGKREYKPPGT
RKLHNILGVETGGPGGRRAGESGHTVADYLKFKDLILRMLDYDPKTRIQPYYALQHSFFK
KTADEGTNTSNSVSTSPAMEQSQSSGTTSSTSSSSGGSSGTSNSGRARSDPTHQHRHSGG
HFTAAVQAMDCETHSPQVRQQFPAPLGWSGTEAPTQVTVETHPVQETTFHVAPQQNALHH
HHGNSSHHHHHHHHHHHHHGQQALGNRTRPRVYNSPTNSSSTQDSMEVGHSHHSMTSLSS
STTSSSTSSSSTGNQGNQAYQNRPVAANTLDFGQNGAMDVNLTVYSNPRQETGIAGHPTY
QFSANTGPAHYMTEGHLTMRQGADREESPMTGVCVQQSPVASS
Function
Dual-specificity kinase which possesses both serine/threonine and tyrosine kinase activities. May play a role in a signaling pathway regulating nuclear functions of cell proliferation. Modulates alternative splicing by phosphorylating the splice factor SRSF6 (By similarity). Exhibits a substrate preference for proline at position P+1 and arginine at position P-3. Has pro-survival function and negatively regulates the apoptotic process. Promotes cell survival upon genotoxic stress through phosphorylation of SIRT1. This in turn inhibits TP53 activity and apoptosis (By similarity).
Reactome Pathway
G0 and Early G1 (R-HSA-1538133 )

Molecular Interaction Atlas (MIA) of This DTT

Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This DTT
43 Patented Agent(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
Benzimidazole DM1IZA7 Cytomegalovirus Disease 1D82 Patented [1]
Harmine DMPA5WD Discovery agent N.A. Patented [1]
PMID28766366-Compound-Scheme11 DMBN3X4 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme12-1 DMMJ5SN N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme12-2 DM3BA1L N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme12-3 DM4V3AY N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme12-4 DM5BG6L N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme13INDY DMLQCYV N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme14BINDY DMBQ0RN N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme15-1 DMVG275 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme15-2 DMU8ENF N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme15-3 DMA423P N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme16DMAT DMQ5UEA N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme18 DMBQ21J N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme1WO2011135259 DMHIUWX N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme21Left DMWTRUK N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme21Right DMF3X40 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme23MPPDerivatives DMRLSKV N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme24-11H-pyrido[4,3-a]carbazole DMBWAV7 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme24Paprotrain DMNKRSZ N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme25-2 DM7OGWH N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme25-3 DMGVT5Y N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme25-4 DMOD9BY N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme27LeucettamineB DM3Q1FT N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme27LeucettineL41 DMLX26R N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme27LeucettineL41derivatives DMPVZ6W N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme2WO2012/098065bottom DMO4Q95 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme2WO2012/098065upper DMVJDRI N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme4Bottom DMDXIU9 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme4Upper DMPH4JV N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme5 DMO6KZ5 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme6Pyrrolo[2,3-d]pyrimidines DMJOG3W N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme7WO2012/098070bottom DMQV6R0 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme7WO2012/098070upper DMGAQR5 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme8NCGC-00010037 DMSX09A N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme8NCGC-00185981 DMDUSN5 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme8NCGC-00189310 DMUWZD9 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme9EHT1610 DMMZGC8 N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme9EHT3356 DMVBPML N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme9EHT5372 DM0O18N N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme9EHT6840 DMVY6PX N. A. N. A. Patented [1]
PMID28766366-Compound-Scheme9EHT9851 DM7RPKM N. A. N. A. Patented [1]
TG003 DMP4HR2 Discovery agent N.A. Patented [1]
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⏷ Show the Full List of 43 Patented Agent(s)
6 Investigative Drug(s) Targeting This DTT
Drug Name Drug ID Indication ICD 11 Highest Status REF
KH-CB19 DMSOB3U Discovery agent N.A. Investigative [2]
leucettine L41 DMBYND6 Discovery agent N.A. Investigative [3]
ML315 DMNOREK Discovery agent N.A. Investigative [4]
PMID23642479C17 DM4JWMA Discovery agent N.A. Investigative [4]
PMID24900699C68 DM2V4MJ Discovery agent N.A. Investigative [5]
WO2013026806C72 DM21WOP Discovery agent N.A. Investigative [6]
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⏷ Show the Full List of 6 Investigative Drug(s)

References

1 Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitors: a survey of recent patent literature.Expert Opin Ther Pat. 2017 Nov;27(11):1183-1199.
2 Specific CLK inhibitors from a novel chemotype for regulation of alternative splicing. Chem Biol. 2011 Jan 28;18(1):67-76.
3 Leucettines, a class of potent inhibitors of cdc2-like kinases and dual specificity, tyrosine phosphorylation regulated kinases derived from the marine sponge leucettamine B: modulation of alternative pre-RNA splicing. J Med Chem. 2011 Jun 23;54(12):4172-86.
4 Small-molecule pyrimidine inhibitors of the cdc2-like (Clk) and dual specificity tyrosine phosphorylation-regulated (Dyrk) kinases: development of chemical probe ML315. Bioorg Med Chem Lett. 2013 Jun15;23(12):3654-61.
5 Tricyclic Pyrimidines As Inhibitors of DYRK1A/DYRK1B As Potential Treatment for Down's Syndrome or Alzheimer's Disease. ACS Med Chem Lett. 2013 Apr 26;4(6):502-3.
6 URL: http://www.guidetopharmacology.org Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Target id: 2009).